WO2007083240A3 - An improved process for the preparation of bisphosphonic acids - Google Patents

An improved process for the preparation of bisphosphonic acids Download PDF

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Publication number
WO2007083240A3
WO2007083240A3 PCT/IB2007/000175 IB2007000175W WO2007083240A3 WO 2007083240 A3 WO2007083240 A3 WO 2007083240A3 IB 2007000175 W IB2007000175 W IB 2007000175W WO 2007083240 A3 WO2007083240 A3 WO 2007083240A3
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WO
WIPO (PCT)
Prior art keywords
preparation
improved process
bisphosphonic acids
acid
bisphosphonic
Prior art date
Application number
PCT/IB2007/000175
Other languages
French (fr)
Other versions
WO2007083240A2 (en
Inventor
Subba Reddy Danda
K A S S Narayan Garimella
Venkata Naga Srinivasa Divvela
Ramesh Dandala
Sivakumaran Meenakshisunderam
Original Assignee
Aurobindo Pharma Ltd
Subba Reddy Danda
K A S S Narayan Garimella
Venkata Naga Srinivasa Divvela
Ramesh Dandala
Sivakumaran Meenakshisunderam
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
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Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=38050916&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=WO2007083240(A3) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Aurobindo Pharma Ltd, Subba Reddy Danda, K A S S Narayan Garimella, Venkata Naga Srinivasa Divvela, Ramesh Dandala, Sivakumaran Meenakshisunderam filed Critical Aurobindo Pharma Ltd
Publication of WO2007083240A2 publication Critical patent/WO2007083240A2/en
Publication of WO2007083240A3 publication Critical patent/WO2007083240A3/en

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/28Phosphorus compounds with one or more P—C bonds
    • C07F9/38Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)]
    • C07F9/3804Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)] not used, see subgroups
    • C07F9/3839Polyphosphonic acids
    • C07F9/3873Polyphosphonic acids containing nitrogen substituent, e.g. N.....H or N-hydrocarbon group which can be substituted by halogen or nitro(so), N.....O, N.....S, N.....C(=X)- (X =O, S), N.....N, N...C(=X)...N (X =O, S)
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/28Phosphorus compounds with one or more P—C bonds
    • C07F9/38Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)]
    • C07F9/3804Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)] not used, see subgroups
    • C07F9/3839Polyphosphonic acids
    • C07F9/386Polyphosphonic acids containing hydroxy substituents in the hydrocarbon radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/553Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
    • C07F9/576Six-membered rings
    • C07F9/58Pyridine rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/645Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having two nitrogen atoms as the only ring hetero atoms
    • C07F9/6503Five-membered rings
    • C07F9/6506Five-membered rings having the nitrogen atoms in positions 1 and 3
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6561Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Biochemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Molecular Biology (AREA)

Abstract

The present invention provides an improved process for the preparation of bisphosphonic acids or salts thereof, e.g alendronic acid, by reacting a carboxylic acid, phosphorus acid and a halophosphorus compound in presence of phenolic compounds as diluent/solvent.
PCT/IB2007/000175 2006-01-20 2007-01-15 An improved process for the preparation of bisphosphonic acids WO2007083240A2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
IN95/CHE/2006 2006-01-20
IN95CH2006 2006-01-20

Publications (2)

Publication Number Publication Date
WO2007083240A2 WO2007083240A2 (en) 2007-07-26
WO2007083240A3 true WO2007083240A3 (en) 2007-10-11

Family

ID=38050916

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/IB2007/000175 WO2007083240A2 (en) 2006-01-20 2007-01-15 An improved process for the preparation of bisphosphonic acids

Country Status (2)

Country Link
US (1) US7528280B2 (en)
WO (1) WO2007083240A2 (en)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8071574B2 (en) 2005-02-22 2011-12-06 John Dennis Bobyn Implant improving local bone formation

Families Citing this family (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2003097655A1 (en) * 2002-05-17 2003-11-27 Teva Pharmaceutical Industries Ltd. Use of certain diluents for making bisphosphonic acids
US8003820B2 (en) * 2005-10-20 2011-08-23 Dr. Reddy's Laboratories Limited Process for preparing bisphosphonic acids
JP5354858B2 (en) * 2006-05-09 2013-11-27 株式会社Adeka Polyester resin composition containing metal salt of sulfonamide compound
US8076483B2 (en) 2006-05-11 2011-12-13 M/S. Ind Swift Laboratories Limited Process for the preparation of pure risedronic acid or salts
AU2007270897A1 (en) * 2006-07-03 2008-01-10 Generics [Uk] Limited Novel process for the preparation of bisphosphonic acids
WO2009050731A2 (en) * 2007-06-20 2009-04-23 Alkem Laboratories Ltd Novel process for preparing risedronic acid
EP2310398A2 (en) 2008-07-11 2011-04-20 Synthon B.V. Process for making 1-hydroxyalkylidene-1,1-biphosphonic acids
US20100075926A1 (en) * 2008-07-23 2010-03-25 Li-Huei Tsai Activation of histone deacetylase 1 (hdac1) protects against dna damage and increases neuronal survival
PL213599B1 (en) 2008-10-31 2013-03-29 Politechnika Gdanska Method of obtaining of [1-hydroxy-2-(1H-imidazole-1-yl)-ethylidene] bisphosphonic acid
US9169279B2 (en) 2009-07-31 2015-10-27 Thar Pharmaceuticals, Inc. Crystallization method and bioavailability
SI2459176T1 (en) 2009-07-31 2018-01-31 Gruenenthal Gmbh Crystallization method and bioavailability
US20160016982A1 (en) 2009-07-31 2016-01-21 Thar Pharmaceuticals, Inc. Crystallization method and bioavailability
WO2011016738A1 (en) 2009-08-05 2011-02-10 Zaklady Farmaceutyczne Polpharma Sa A process for the synthesis of 1-hydroxy-3-(n-methylpentylamino) propylidene bisphosphonic acid monosodium salt, monohydrate
EA201270328A1 (en) 2009-08-28 2012-09-28 Синтон Б. В. METHOD OF OBTAINING 1-HYDROXYLKYLIDENE-1,1-DIPHOSPHONE ACIDS
US9340565B2 (en) 2010-11-24 2016-05-17 Thar Pharmaceuticals, Inc. Crystalline forms
CA2842524C (en) 2011-07-22 2020-07-14 Massachusetts Institute Of Technology Activators of class i histone deacetylases (hdacs) and uses thereof
WO2017208070A1 (en) 2016-05-31 2017-12-07 Grünenthal GmbH Bisphosphonic acid and coformers with lysin, glycin, nicotinamide for treating psoriatic arthritis

Citations (3)

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US2957931A (en) * 1949-07-28 1960-10-25 Socony Mobil Oil Co Inc Synthesis of compounds having a carbonphosphorus linkage
WO2002090367A1 (en) * 2001-05-10 2002-11-14 Eos Eczacibasi Ozgun Kimyasal Urunler Sanayi Ve Ticaret A.S. Process for the preparation of 4-amino-1-hydroxybutylidene-1, 1-biphosphonic acid
US20060258625A1 (en) * 2006-02-20 2006-11-16 Alembic Limited Process for the preparation of biphosphonic derivatives

Family Cites Families (15)

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DE2654112C2 (en) * 1976-11-29 1984-10-04 Bayer Ag, 5090 Leverkusen Polycondensates
DE3016289A1 (en) 1980-04-28 1981-10-29 Henkel KGaA, 4000 Düsseldorf METHOD FOR PRODUCING OMEGA-AMINO-1-HYDROXYALKYLIDEN-1,1-BIS-PHOSPHONIC ACIDS
IT1196315B (en) 1984-10-29 1988-11-16 Gentili Ist Spa PROCEDURE FOR THE PREPARATION OF DIPHOSPHONIC ACIDS
US4922007A (en) 1989-06-09 1990-05-01 Merck & Co., Inc. Process for preparing 4-amino-1-hydroxybutylidene-1,1-bisphosphonic acid or salts thereof
US5019651A (en) 1990-06-20 1991-05-28 Merck & Co., Inc. Process for preparing 4-amino-1-hydroxybutylidene-1,1-bisphosphonic acid (ABP) or salts thereof
US5510517A (en) 1993-08-25 1996-04-23 Merck & Co., Inc. Process for producing N-amino-1-hydroxy-alkylidene-1,1-bisphosphonic acids
CA2197267C (en) 1997-02-11 2000-02-08 Yong Tao Process for the production of 4-amino-1-hydroxybutylidene-1,1-bisphosphonic acid or salts thereof
BR0010112A (en) * 1999-02-17 2001-12-26 Teva Pharma Process for preparing alendronic acid
ES2153794B1 (en) 1999-08-06 2001-10-16 Medichem Sa PROCEDURE FOR OBTAINING THE 4-AMINO-1-HYDROXIBUTILIDEN-1,1-BISPHOSPHONIC ACID AND ITS TRIHYDRATED MONOSODIC SALT.
ITMI20020908A1 (en) * 2002-04-29 2003-10-29 Chemi Spa ALENDRONATE SODIUM PREPARATION PROCESS
WO2003097655A1 (en) 2002-05-17 2003-11-27 Teva Pharmaceutical Industries Ltd. Use of certain diluents for making bisphosphonic acids
WO2005044831A2 (en) 2003-08-21 2005-05-19 Sun Pharmaceutical Industries Limited A process for preparation of bisphosphonic acid compounds
US7361761B2 (en) 2004-09-28 2008-04-22 Orchid Chemicals & Pharmaceuticals Ltd. Process for the preparation of bisphosphonic acid
PL199215B1 (en) 2004-12-28 2008-08-29 Politechnika Gdanska Method for the manufacture of [1-hydroxy-2-(3-pyridyl) ethylidene bis-phosphonic] acid and its 2 and a half aqueous monosodium salt
US8003820B2 (en) 2005-10-20 2011-08-23 Dr. Reddy's Laboratories Limited Process for preparing bisphosphonic acids

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2957931A (en) * 1949-07-28 1960-10-25 Socony Mobil Oil Co Inc Synthesis of compounds having a carbonphosphorus linkage
WO2002090367A1 (en) * 2001-05-10 2002-11-14 Eos Eczacibasi Ozgun Kimyasal Urunler Sanayi Ve Ticaret A.S. Process for the preparation of 4-amino-1-hydroxybutylidene-1, 1-biphosphonic acid
US20060258625A1 (en) * 2006-02-20 2006-11-16 Alembic Limited Process for the preparation of biphosphonic derivatives

Non-Patent Citations (1)

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Title
JÜBERMANN, O.: "Houben- Weyl; Methoden der organischen Chemie, Band I/1, Allgemeine Laboratoriumspraxis I; Auswahl der Lösungsmittel", 1958, G. THIEME VERLAG, DE, STUTTGART, XP002435464 *

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8071574B2 (en) 2005-02-22 2011-12-06 John Dennis Bobyn Implant improving local bone formation

Also Published As

Publication number Publication date
WO2007083240A2 (en) 2007-07-26
US20070173645A1 (en) 2007-07-26
US7528280B2 (en) 2009-05-05

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